Rozulip tablets p/o 10mg №7×4

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Rozulip tabl p/o 10mg in bl. in pack. No. 7×4
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Film-coated tablets, white or almost white, round, biconvex, engraved with “E” on one side and the number “592” on the other, odorless or almost odorless. The main active ingredient Rosuvastatin Release form Film-coated tablets of white or almost white color, round, biconvex, engraved “E” on one side and the number “592” on the other, odorless or almost odorless. Dosage 10mg in bl. in pack. No. 7×4 Special instructions When using the drug Rozulip® at a dose of 40 mg, it is recommended to monitor indicators of kidney function. With the use of the drug Rozulip® in all doses, especially more than 20 mg, the development of myalgia, myopathy and, in rare cases, rhabdomyolysis has been reported. Determination of CPK activity should not be carried out after intense physical exertion or in the presence of other possible reasons for an increase in CPK activity, which may lead to incorrect interpretation of the results. If the initial activity of CPK is significantly increased (5 times higher than the upper limit of the norm), after 5-7 days a second measurement should be taken. You should not start therapy if a repeat test confirms an increased activity of CPK (5 times higher than ULN). When prescribing Rozulip® (as well as other HMG-CoA reductase inhibitors) in patients with existing risk factors for rhabdomyolysis, it is necessary to consider the ratio of expected benefit and potential risk and conduct clinical observation. The patient should be informed about the need to immediately inform the doctor about cases of sudden onset of muscle pain, muscle weakness or spasms, especially in combination with malaise and fever. In such patients, CPK activity should be determined. Therapy should be discontinued if CPK activity is significantly increased (more than 5 times compared to ULN) or if muscle symptoms are pronounced and cause daily discomfort (even if CPK activity is 5 times less compared to ULN). If symptoms disappear and CPK activity returns to normal, consideration should be given to re-prescribing Rozulip or other HMG-CoA reductase inhibitors at lower doses with careful monitoring of the patient. Routine monitoring of CPK activity in the absence of symptoms is impractical. There were no signs of an increase in toxic effects on skeletal muscles when using Rosulip® as part of combination therapy. An increase in the incidence of myositis and myopathy has been reported in patients taking other HMG-CoA reductase inhibitors in combination with fibric acid derivatives (including gemfibrozil), cyclosporine, nicotinic acid in lipid-lowering doses (more than 1 g / day), azole antifungals, inhibitors proteases and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when administered concomitantly with certain HMG-CoA reductase inhibitors. Thus, the simultaneous administration of the drug Rozulip® and gemfibrozil is not recommended. The ratio of the expected benefit and potential risk should be carefully weighed when using the drug Rozulip® and fibrates or nicotinic acid in lipid-lowering doses (more than 1 g / day). 2-4 weeks after the start of treatment and / or with an increase in the dose of Rozulip®, it is necessary to monitor lipid metabolism (if necessary, dose adjustment is required). It is recommended to determine the activity of transaminases before the start of therapy and 3 months after the start of therapy. Reception of the drug Rozulip® should be discontinued or the dose of the drug should be reduced if the activity of transaminases in the blood serum is 3 times higher than the upper limit of the norm. In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of the underlying diseases should be carried out before starting treatment with Rozulip®. Clinical experience and data on the use of the drug in patients with impaired liver function, corresponding to more than 9 points on the Child-Pugh scale, are not available. Very rare cases of interstitial lung disease have been reported in patients treated with certain statin drugs. As a rule, these cases were observed during long-term therapy with statins. Interstitial lung disease is manifested by shortness of breath, non-productive cough and deterioration in general condition (fatigue, weight loss and fever). If interstitial lung disease is suspected, statin therapy should be discontinued. The results of pharmacokinetic studies indicate that in patients of the Mongoloid race, the bioavailability of rosuvastatin is higher than in the representatives of the Caucasian race. Rosulip® should not be taken by patients with lactose intolerance, lactase deficiency or glucose-galactose malabsorption, because. the product contains lactose. Use in pediatrics The efficacy and safety of the drug in children and adolescents under the age of 18 years has not been established. The experience of using the drug in pediatric practice is limited to a small number of children (8 years and older) with familial homozygous hypercholesterolemia. It is currently not recommended to use Rozulip® in children. Influence on the ability to drive vehicles and control mechanisms Patients should be careful when driving vehicles or work that requires increased concentration and speed of psychomotor reaction, dizziness may occur during therapy. Pharmacological action Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, which is a precursor of cholesterol (Xc). Rosuvastatin increases the number of LDL receptors on the surface of liver cells, which increases the absorption and catabolism of LDL, and also suppresses the synthesis of VLDL in the liver. As a result, the total number of VLDL and LDL particles is reduced. Reduces the elevated concentration of low-density lipoprotein cholesterol (Xc-LDL), total cholesterol and triglycerides, and also increases the concentration of high-density lipoprotein cholesterol (Xc-HDL). In addition, rosuvastatin reduces the concentration of apolipoprotein B (ApoB), non-HDL cholesterol (Xc-non-HDL), very low density lipoprotein cholesterol (Xc-VLDL), very low density lipoprotein triglycerides (TG-VLDL) and increases the content of apolipoprotein AI (ApoA-I ). Rosuvastatin also reduces the ratio of Xc-LDL / Xc-HDL, total cholesterol / Xc-HDL, Xc-non-HDL / Xc-HDL and ApoB / ApoA-I. The therapeutic effect of the drug appears within one week after the start of treatment. For 2 weeks of therapy, the effectiveness reaches a level that is 90% of the maximum possible. The maximum therapeutic effect is usually achieved by the 4th week of therapy and is maintained with regular intake. The safety and efficacy of rosuvastatin in the pediatric population have not been proven. For this category of patients, the experience of using the drug is limited to a small number of patients (aged 8 years and older) with homozygous hereditary hypercholesterolemia. Pharmacokinetics Absorption Cmax of rosuvastatin in blood plasma is achieved approximately 5 hours after ingestion. The absolute bioavailability of the drug is about 20%. Distribution Rosuvastatin is extensively absorbed by the liver, where the main synthesis of cholesterol and excretion of LDL-C occurs. Vd of rosuvastatin reaches 134 liters. Approximately 90% of rosuvastatin binds to plasma proteins, mainly to albumin. Metabolism Rosuvastatin undergoes limited metabolism (about 10%) in the liver. It is a non-core substrate for isoenzymes of the cytochrome P450 system. The main isoenzyme involved in the metabolism of rosuvastatin is CYP2C9. Isoenzymes CYP2C19, CYP3A4 and CYP2D6 are less involved in metabolism. The main identified metabolites of rosuvastatin are N-desmethyl and lactone metabolites. N-desmethyl is about 50% less active than rosuvastatin, lactone metabolites are pharmacologically inactive. More than 90% of the pharmacological activity of inhibiting circulating HMG-CoA reductase is provided by rosuvastatin, the rest is its metabolites. Withdrawal Approximately 90% of the dose of rosuvastatin is excreted unchanged through the intestines. Approximately 5% of the drug dose is excreted by the kidneys unchanged. T1 / 2 drug from blood plasma is approximately 19 hours and does not change with increasing doses of the drug. Plasma clearance of rosuvastatin reaches an average of 50 l / h (coefficient of variation – 21.7%). As with other HMG-CoA reductase inhibitors, the hepatic uptake of rosuvastatin involves the membrane cholesterol transporter, which plays an important role in the hepatic elimination of rosuvastatin. The systemic bioavailability of rosuvastatin increases in proportion to the dose. When using the drug several times a day, pharmacokinetic parameters do not change. Pharmacokinetics in special groups of patients Gender and age do not have a clinically significant effect on the pharmacokinetics of rosuvastatin. Pharmacokinetic studies have shown an approximately two-fold increase in the median AUC and Cmax of rosuvastatin in plasma in patients of the Mongoloid race (Japanese, Chinese, Filipinos, Vietnamese and Koreans) compared with Caucasians; in Indian patients, an increase in the median AUC and Cmax by 1.3 times was shown. The analysis did not reveal clinically significant differences in pharmacokinetics between Caucasians and Blacks. In patients with mild to moderate renal insufficiency, the plasma concentration of rosuvastatin or N-desmethyl does not change significantly. In patients with severe renal insufficiency (CC less than 30 ml / min), the concentration of rosuvastatin in plasma is 3 times higher, and the concentration of N-desmethyl is 9 times higher than in healthy volunteers. The plasma concentration of rosuvastatin in patients on hemodialysis was approximately 50% higher than in healthy volunteers. In patients with various stages of liver failure, an increase in T1 / 2 of rosuvastatin was not detected (patients with a score of 7 or lower on the Child-Pugh scale). In 2 patients with scores of 8 and 9 on the Child-Pugh scale, an increase in T1 / 2 was noted, at least 2 times. There is no experience with the use of rosuvastatin in patients with a score above 9 on the Child-Pugh scale. Indications Primary hypercholesterolemia (Fredrickson type IIa) or mixed hypercholesterolemia (Fredrickson type IIb) as an adjunct to diet when diet and other non-drug treatments (eg, exercise, weight loss) are inadequate; – homozygous hereditary hypercholesterolemia as an adjunct to diet and other treatments aimed at lowering blood lipids (for example, LDL apheresis), as well as in cases where these methods are not effective enough; – hypertriglyceridemia (Fredrickson type IV) as an addition to the diet; – to slow down the progression of atherosclerosis as an addition to the diet in patients, incl. those who are indicated for therapy to reduce the level of total cholesterol and cholesterol-LDL; – prevention of major cardiovascular complications (stroke, myocardial infarction, arterial revascularization) in adult patients without clinical signs of coronary artery disease, but with an increased risk of its development (age over 50 years for men and over 60 years for women, increased concentration of C-reactive protein (≤2 mg/l) in the presence of at least one of the additional risk factors, such as arterial hypertension, low concentration of HDL-C, smoking, indication of a family history of early onset of coronary artery disease). Dosage and administration The drug is taken orally. The tablet should be swallowed whole with water, without chewing or crushing. Rozulip® can be taken at any time of the day, regardless of food intake. Before starting treatment with Rozulip®, the patient should be prescribed a standard low cholesterol diet. The patient must follow the diet during the entire course of therapy. The dose of the drug should be selected individually depending on the indication and therapeutic response to treatment, taking into account current recommendations for target lipid levels. The recommended initial dose of Rozulip® for patients starting to take the drug, or for patients transferred from taking other HMG-CoA reductase inhibitors, is 5 or 10 mg 1 time / day. When choosing an initial dose, one should be guided by the patient’s cholesterol level and take into account the risk of developing cardiovascular complications, and it is also necessary to evaluate the potential risk of side effects. If necessary, the dose may be increased after 4 weeks. After using for 4 weeks a dose exceeding the recommended initial dose, a subsequent increase to 40 mg can be carried out only in patients with severe hypercholesterolemia and at high risk of cardiovascular complications (especially in patients with familial hypercholesterolemia) who have not achieved the desired the result of therapy when used at a dose of 20 mg, and which will be under the supervision of a specialist. Particularly careful monitoring of patients receiving the drug at a dose of 40 mg is recommended. For the treatment of patients over 65 years of age, the recommended initial dose is 5 mg. There is no need for other changes in the dose of the drug associated with the age of patients. Patients with mild or moderate renal insufficiency dose adjustment is not required. For patients with moderate renal impairment (CC less than 60 ml / min), an initial dose of 5 mg is recommended. The 40 mg dose is contraindicated in patients with moderate renal impairment. In severe renal insufficiency, the drug Rozulip® is contraindicated in any doses. When prescribing the drug in doses of 10 mg and 20 mg, the recommended initial dose for patients of the Mongoloid race is 5 mg. The appointment of the drug at a dose of 40 mg to patients of the Mongoloid race is contraindicated. When prescribing the drug in doses of 10 mg and 20 mg, the recommended initial dose for patients predisposed to myopathy is 5 mg. The appointment of the drug at a dose of 40 mg is contraindicated in patients with factors that may indicate a predisposition to the development of myopathy. After 2-4 weeks of therapy and / or with an increase in the dose of Rozulip®, it is necessary to monitor lipid metabolism, if necessary, dose adjustment is required. Use during pregnancy and lactationRozulip® is contraindicated during pregnancy and lactation (breastfeeding). When diagnosing pregnancy during therapy, the use of the drug should be discontinued immediately. Women of reproductive age should use adequate methods of contraception. Since Xc and its biosynthetic products are important for fetal development, the potential risk of HMG-CoA reductase inhibition outweighs the benefits of using the drug. There are no data on the excretion of rosuvastatin in breast milk, therefore, if necessary, the use of the drug during lactation, breastfeeding should be discontinued. Precautions Caution should be used in the form of 10 mg and 20 mg tablets if there is a risk of developing myopathy / rhabdomyolysis – renal failure, hypothyroidism, a personal or family history of hereditary muscle diseases, a history of muscle toxicity when using other HMG inhibitors -CoA reductase or fibrates; with excessive alcohol consumption; in patients over the age of 65; conditions in which an increase in the plasma concentration of rosuvastatin is noted; in patients of the Mongoloid race; simultaneously with fibrates; with a history of liver disease; sepsis; arterial hypotension; extensive surgical interventions, injuries; with severe metabolic, endocrine or electrolyte disorders or uncontrolled seizures. With caution, the drug in the form of 40 mg tablets should be used in patients with mild renal insufficiency (CC more than 60 ml / min); over the age of 65; with a history of liver disease; sepsis; arterial hypotension; major surgery, trauma, severe metabolic, endocrine or electrolyte disturbances, or uncontrolled seizures. Interaction with other drugs Cyclosporine: with the simultaneous use of rosuvastatin and cyclosporine, the AUC of rosuvastatin was on average 7 times higher than the value observed in healthy volunteers. Simultaneous use leads to an increase in the concentration of rosuvastatin in the blood plasma by 11 times, while the plasma concentration of cyclosporine does not change. Vitamin K antagonists: initiation of therapy with rosuvastatin or an increase in the dose of the drug in patients receiving concomitant vitamin K antagonists (for example, warfarin) may lead to an increase in prothrombin time and MHO. Cancellation of rosuvastatin or a decrease in its dose may lead to a decrease in MHO. In such cases, MHO monitoring is recommended. Gemfibrozil and lipid-lowering agents: The combined use of rosuvastatin and gemfibrozil leads to a 2-fold increase in plasma Cmax and AUC of rosuvastatin. Possible pharmacodynamic interaction. Gemfibrozil, other fibrates, and nicotinic acid at lipid-lowering doses (more than 1 g/day) increased the risk of myopathy when used concomitantly with other HMG-CoA reductase inhibitors, possibly due to the fact that they can cause myopathy when used as monotherapy. While taking the drug with gemfibrozil, fibrates, nicotinic acid in lipid-lowering doses (more than 1 g / day), patients are recommended an initial dose of 5 mg. Therapy with rosuvastatin at a dose of 40 mg is contraindicated with the concomitant use of fibrates. Ezetimibe: the simultaneous use of the drug Rozulip® and ezetimibe was not accompanied by a change in the AUC and Cmax of both drugs. However, a pharmacodynamic interaction with the development of side effects cannot be ruled out between rosuvastatin and ezetimibe. HIV protease inhibitors: Although the exact mechanism of interaction is unknown, co-administration of HIV protease inhibitors can lead to a significant increase in exposure to rosuvastatin. A pharmacokinetic study on the simultaneous use of 20 mg rosuvastatin with a combination preparation containing two protease inhibitors (400 mg lopinavir / 100 mg ritonavir) in healthy volunteers resulted in an approximately two-fold and five-fold increase in AUC (0-24) and Cmax of rosuvastatin, respectively. Therefore, concomitant use of rosuvastatin and protease inhibitors is not recommended in the treatment of patients with HIV. Antacids: The simultaneous use of rosuvastatin and suspensions of antacids containing aluminum and magnesium hydroxide leads to a decrease in the plasma concentration of rosuvastatin by approximately 50%. This effect is less pronounced if the antacid suspension is applied 2 hours after taking rosuvastatin. The clinical significance of this interaction has not been studied. Erythromycin: The simultaneous use of rosuvastatin and erythromycin leads to a decrease in the AUC of rosuvastatin by 20% and the Cmax of rosuvastatin by 30%, probably as a result of increased intestinal motility caused by erythromycin. Oral contraceptives / hormone replacement therapy (HRT): the simultaneous use of rosuvastatin and oral contraceptives increases the AUC of ethinyl estradiol and the AUC of norgestrel by 26% and 34%, respectively. Such an increase in plasma concentration should be taken into account when selecting a dose of oral contraceptives against the background of the use of Rozulip. Pharmacokinetic data on the simultaneous use of Rozulip and HRT are not available, therefore, a similar effect cannot be excluded when using this combination. However, this combination was widely used during clinical trials and was well tolerated by patients. Other medicinal products: no clinically significant interaction of rosuvastatin with digoxin is expected. Cytochrome P450 isoenzymes: In vivo and in vitro studies have shown that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a weak substrate for these isoenzymes. There was no clinically significant interaction between rosuvastatin and fluconazole (an inhibitor of CYP2C9 and CYP3A4 isoenzymes) and ketoconazole (an inhibitor of CYP2A6 and CYP3A4 isoenzymes). The combined use of rosuvastatin and itraconazole (an inhibitor of the CYP3A4 isoenzyme) increases the AUC of rosuvastatin by 28% (clinically insignificant). Thus, an interaction associated with the cytochrome P450 system is not expected. Contraindications – liver disease in the active phase, including a persistent increase in serum transaminase activity and any increase in serum transaminase activity (more than 3 times compared with VGN); – severe renal dysfunction (CC less than 30 ml / min); – myopathy; – simultaneous reception of cyclosporine; – pregnancy; – lactation period; – lack of adequate methods of contraception in women with preserved reproductive function; – predisposition to the development of myotoxic complications; – children and adolescents under 18 years of age (due to the lack of sufficient clinical data, efficacy and safety have not been established); – lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose); – hypersensitivity to rosuvastatin and other components of the drug. Composition In 1 tab. rosuvastatin zinc 10.68 mg, which corresponds to the content of rosuvastatin 10 mg Shell composition: Opadry II white 85F18422 – 3.8 mg (polyvinyl alcohol (40%), titanium dioxide (25%), macrogol 3350 (20.2%), talc (14.8%)). Overdose Treatment: There is no specific antidote. It is recommended to carry out symptomatic treatment and measures aimed at maintaining the functions of vital organs and systems. It is necessary to monitor liver function and serum CPK levels. The effectiveness of hemodialysis is unlikely. Side effects During therapy with rosuvastatin, predominantly mild and transient adverse reactions were recorded. As with other HMG-CoA reductase inhibitors, the frequency of adverse reactions associated with rosuvastatin therapy is dose dependent. Classification of adverse reactions depending on the frequency of occurrence: often (from> 1/100 to <1/10), infrequently (from> 1/1000 to <1/100), rarely (from> 1/10,000 to <1/1000 ), very rare (<1/10,000), frequency unknown (cannot be determined from the available data). From the immune system: rarely - hypersensitivity reactions, including angioedema. From the nervous system: often - headache, dizziness; very rarely - polyneuropathy, loss or decrease in memory. From the digestive system: often - constipation, nausea, abdominal pain; infrequently - a slight, asymptomatic, transient increase in liver transaminase activity; rarely - pancreatitis; very rarely - jaundice, hepatitis; frequency unknown - diarrhea. From the skin and subcutaneous structures: infrequently - itching, rash and urticaria; frequency unknown - Stevens-Johnson syndrome. From the musculoskeletal system: often - myalgia; rarely - myopathy (including myositis) and rhabdomyolysis with or without acute renal failure; frequency unknown - immune-mediated necrotizing myopathy. A dose-dependent increase in CPK concentration was observed in a small number of patients taking rosuvastatin. In most cases, it was minor, asymptomatic and temporary. In the event of an increase in the concentration of CK more than 5 times higher than the upper limit of the norm, therapy should be suspended. Very rarely - arthralgia. From the urinary system: proteinuria (less than 1% of patients receiving a dose of 10-20 mg and about 3% of patients receiving a dose of 40 mg). In most cases, proteinuria decreases or disappears during therapy and does not indicate the onset of acute or progression of existing kidney disease. Very rarely - hematuria. From the respiratory system: the frequency is unknown - cough, shortness of breath. On the part of laboratory parameters: rarely - thrombocytopenia; the frequency is unknown - hyperglycemia, an increase in the concentration of glycated hemoglobin, bilirubin, GGT activity, alkaline phosphatase. Others: often - asthenic syndrome; very rarely - gynecomastia; the frequency is unknown - thyroid dysfunction is possible. The following adverse events have been reported during therapy with some statins: the frequency is unknown - sleep disturbances, including insomnia and nightmares, depression; sexual dysfunction, isolated cases of interstitial lung disease (especially with prolonged use). Storage conditions The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C. Buy Rosulip tablets p/o 10mg №7x4 Price for Rosulip tablets p/o 10mg №7x4